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Assay Detail

CHEMBL871977

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Displacement of [3H]-Rolipram from mouse brain homogenates
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Tissue Brain
Confidence 5 — Multiple protein complex / RNA
Curated By Expert

Target

Phosphodiesterase 4 (CHEMBL2111373)
Type PROTEIN FAMILY
Organism Mus musculus

Publication

Synthesis and in vitro profile of a novel series of catechol benzimidazoles. The discovery of potent, selective phosphodiesterase type IV inhibitors with greatly attenuated affinity for the [3H]rolipram binding site
Cheng JB, Cooper K, Duplantier AJ, Eggler JF, Kraus KG, Marshall SC, Marfat A, Masamune H, Shirley JT, Tickner JE, Umland JP
Bioorg Med Chem Lett (1995) 5 : 1969 -1972
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.97 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL63 ROLIPRAM 2.0 1 8.40
CHEMBL58915 1 7.50
CHEMBL294883 1 7.11
CHEMBL59269 1 6.89
CHEMBL291537 1 6.66
CHEMBL60073 1 5.23

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL63 ROLIPRAM IC50 = 4.0 nM 8.40
CHEMBL58915 IC50 = 32.0 nM 7.50
CHEMBL294883 IC50 = 78.0 nM 7.11
CHEMBL59269 IC50 = 130.0 nM 6.89
CHEMBL291537 IC50 = 220.0 nM 6.66
CHEMBL60073 IC50 = 5910.0 nM 5.23